Health & Environmental Research Online (HERO)


Print Feedback Export to File
7357291 
Journal Article 
Synthesis and cytotoxicity of new thiazolo[4,5-b]pyridine-2(3H)-one derivatives based on alpha,beta-unsaturated ketones and alpha-ketoacids 
Lozynskyi, A; Zimenkovsky, B; Radko, L; Stypula-Trebas, S; Roman, O; Gzella, AK; Lesyk, R 
2018 
Yes 
Chemical Papers / Chem Zvesti
ISSN: 0366-6352
EISSN: 1336-9075 
72 
669-681 
A series of thiazolo[4,5-b]pyridin-2(3H)-one derivatives were obtained via [3 + 3]-cyclization of 4-amino-5H-thiazol-2-one and alpha,beta-unsaturated ketones or alpha-ketoacids. The structures of newly synthesized compounds were established by spectral data and a single-crystal X-ray diffraction analysis. Target compounds were screened for their anticancer activity according to US NCI protocols and moderate inhibitory activity against the tested cell line was confirmed. 5-Phenyl-7-(pyridin-3-yl)-3H-thiazolo[4,5-b]pyridin-2-one (3) and 2-oxo-7-thiophen-2-yl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (12) were screened for their cytotoxicity effects on HepG2 and Balb/c 3T3 cells which revealed promising results using MTT, NRU and TPC assays. [GRAPHICS] . 
4-Amino-5H-thiazol-2-one; Thiazolo[4,5-b]pyridin-2(3H)-one; X-ray study; Cell lines; HepG2; Balb/c 3T3